GPR39-C3 --- GPR39 Agonist


Catalog No. size PriceQuantity
M60209-2S 2 mg solid $99
M60209-10S 10mg solid $180

Description

GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC50 ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39. It has no inhibitory effects (at 10 μM) on a panel of kinases and exhibits no relevant binding affinity for the related ghrelin and neurotensin-1 receptors and other enzymes, transporters, and GPCRs. GPR39-C3 has excellent functional activity in physiologically relevant rodent cells and in vivo. An acute study in normal mice with orally administrated GPR39-C3 confirmed in vitro findings by demonstrating an increase of the relevant pharmacodynamic marker GLP-1. It is a good chemical tool to enable interrogation of GPR39 signaling in different cellular contexts.

Product information

CAS Number: 1621175-65-2

Molecular Weight: 418.90

Formula: C18H19ClN6O2S

Chemical Name: N-(3-chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide

Smiles: CNC1=NC(=CC(NCC2=CC=C(C=C2Cl)NS(C)(=O)=O)=N1)C1=CC=CC=N1

InChiKey: DRSZMILOMUPIBJ-UHFFFAOYSA-N

InChi: InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GPR39-C3 was used at 0.1-1 µM final concentration in various in vitro assays.

In Vivo:

GPR39-C3 was dosed to Male C57BL/6 mice via oral gavage at 30 mg/kg, concurrently with DPP4 inhibitor PKF275-055 (3 mg/kg). The animals were challenged orally after 1 hour with a glucose bolus (3 g/kg) and active GLP-1 levels were measured 30 min later by MSD Active GLP-1 Assay kit. Formulation is 0.5% methylcellulose/0.1% Tween 80 in water.

References:

  1. Bassilana F, et al. Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39. (2014) Nat Chem Biol. 10(5):343-9.
  2. Stefan Peukert, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. (2014) ACS Med. Chem. Lett. In press.

Products are for research use only. Not for human use.


Documents

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed